Salbutamol was patented in 1966 in Britain and became commercially available in the UK in 1969.[10][11] It was approved for medical use in the United States in 1982.[6] It is on the World Health Organization's List of Essential Medicines, which lists the most effective and safe medicines needed in a health system.[12] Salbutamol is available as a generic medication.[6] The wholesale cost in the developing world of an inhaler which contains 200 doses is between US$1.12 and US$2.64 as of 2014.[13] In the United States, it is between US$25 and US$50 for a typical month's supply.[14] In 2016, it was the 10th most prescribed medication in the United States, with more than 47 million prescriptions.[15]

The tertiary butyl group in salbutamol makes it more selective for β2 receptors,[19] which are the predominant receptors on the bronchial smooth muscles. Activation of these receptors causes adenylyl cyclase to convert ATP to cAMP, beginning the signalling cascade that ends with the inhibition of myosin phosphorylation and lowering the intracellular concentration of calcium ions (myosin phosphorylation and calcium ions are necessary for muscle contractions). The increase in cAMP also inhibits inflammatory cells in the airway, such as basophils, eosinophils, and most especially mast cells, from releasing inflammatory mediators and cytokines.[20][21] Salbutamol and other β2 receptor agonists also increase the conductance of channels sensitive to calcium and potassium ions, leading to hyperpolarization and relaxation of bronchial smooth muscles.[22]

Salbutamol is either filtered out by the kidneys directly or is first metabolized into 4'-O-sulphate, which is excreted in the urine.[8]

Salbutamol is sold as a racemic mixture. The (R)-(−)-enantiomer (CIP nomenclature) is shown in the image at right (top), and is responsible for the pharmacologic activity; the (S)-(+)-enantiomer (bottom) blocks metabolic pathways associated with elimination of itself and of the pharmacologically active enantiomer (R).[23] The slower metabolism of the (S)-(+)-enantiomer also causes it to accumulate in the lungs, which can cause airway hyperreactivity and inflammation.[24]

The 1972 Munich Olympics were the first Olympics where anti-doping measures were deployed, and at that time beta-2 agonists were considered to be stimulants with high risk of abuse for doping. Inhaled salbutamol was banned from those games, but by 1986 was permitted (although oral beta-2 agonists were not). After a steep rise in the number of athletes taking beta-2 agonists for asthma in the 1990s, Olympic athletes were required to provide proof that they had asthma in order be allowed to use inhaled beta-2 agonists.[26]

The wholesale cost of a 200-dose inhaler is between US$1.12 and US$2.64 in the developing world as of 2014[update][13] and GB£1.50 in the United Kingdom as of 2015[update].[27] In the United States, a typical month's supply is between $25 and $50.[14]

Salbutamol is the INN (international nonproprietary name) while albuterol is the USAN (United States adopted name). The drug is usually manufactured and distributed as the sulphatesalt (salbutamol sulphate).

It was first sold by Allen & Hanburys (UK) under the brand name Ventolin, and has been used for the treatment of asthma ever since.[28] The drug is marketed under many names worldwide.[3]

As of 2011[update] there was no evidence that an increase in physical performance occurs after inhaling salbutamol, but various reports for benefit when delivered orally or intravenously.[29][30] In spite of this, salbutamol required "a declaration of Use in accordance with the International Standard for Therapeutic Use Exemptions" under the 2010 WADA prohibited list. This requirement was relaxed when the 2011 list was published to permit the use of "salbutamol (maximum 1600 micrograms over 24 hours) and salmeterol when taken by inhalation in accordance with the manufacturers’ recommended therapeutic regimen."[31][32]

Abuse of the drug may be confirmed by detection of its presence in plasma or urine, typically exceeding 1000 ng/mL. The window of detection for urine testing is on the order of just 24 hours, given the relatively short elimination half-life of the drug,[33][34][35] estimated at between 5 and 6 hours following oral administration of 4 mg.[20]

Salbutamol's low toxicity makes it safe for other animals and thus is the medication of choice for treating acute airway obstruction in most species.[24] It is usually used to treat bronchospasm or coughs in cats and dogs and used as a bronchodilator in horses with recurrent airway obstruction; it can also be used in emergencies to treat asthmatic cats.[39][40]

Toxic effects require an extremely high dose, and most overdoses are due to dogs chewing on and puncturing an inhaler or nebulizer vial.[41]